U.S. patent application number 14/628626 was filed with the patent office on 2015-08-27 for highly soluble purine bioactive compounds and compositions thereof.
The applicant listed for this patent is JHO Intellectual Property Holdings, LLC. Invention is credited to Jack Owoc.
Application Number | 20150238494 14/628626 |
Document ID | / |
Family ID | 53881176 |
Filed Date | 2015-08-27 |
United States Patent
Application |
20150238494 |
Kind Code |
A1 |
Owoc; Jack |
August 27, 2015 |
HIGHLY SOLUBLE PURINE BIOACTIVE COMPOUNDS AND COMPOSITIONS
THEREOF
Abstract
The invention provides nutritional supplements, in powder,
tablet or capsule dosage forms and aqueous formulations, containing
one or more of the purine bioactive compounds described including
theacrine and theacrine species.
Inventors: |
Owoc; Jack; (Weston,
FL) |
|
Applicant: |
Name |
City |
State |
Country |
Type |
JHO Intellectual Property Holdings, LLC |
Davie |
FL |
US |
|
|
Family ID: |
53881176 |
Appl. No.: |
14/628626 |
Filed: |
February 23, 2015 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
|
|
61944528 |
Feb 25, 2014 |
|
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Current U.S.
Class: |
424/94.1 ;
514/21.2; 514/263.32 |
Current CPC
Class: |
A23V 2002/00 20130101;
A23L 2/52 20130101; A61K 31/00 20130101; A23V 2002/00 20130101;
A23L 2/02 20130101; A61K 45/06 20130101; A61K 9/0095 20130101; A61K
9/4858 20130101; A61K 31/522 20130101; A61K 9/0019 20130101; A23V
2250/712 20130101; A61K 2300/00 20130101; A23V 2250/21 20130101;
A23V 2250/54246 20130101; A23V 2250/062 20130101; A23V 2250/5108
20130101; A23V 2250/704 20130101; A23V 2250/54252 20130101; A23V
2200/31 20130101; A23V 2250/5118 20130101; A23L 33/10 20160801;
A61K 31/522 20130101 |
International
Class: |
A61K 31/522 20060101
A61K031/522; A61K 9/00 20060101 A61K009/00; A23L 2/44 20060101
A23L002/44; A23L 2/66 20060101 A23L002/66; A23L 2/38 20060101
A23L002/38; A23L 2/02 20060101 A23L002/02; A61K 45/06 20060101
A61K045/06; A23L 2/52 20060101 A23L002/52 |
Claims
1. Stable aqueous compositions for oral administration of at least
one biologically-active form of a purine alkaloid compound
structurally related to caffeine to a mammalian subject, which
compositions comprise: a) 1,3,7,9-tetramethyluric acid (theacrine),
(O(2), 2-Methoxy-1,9-dimethyl-7H-purine-6,8-dione (liberine) and
(O(2), 1,7,9-trimethyluric acid (methylliberine), said liberine and
methylliberine collectively referred to as theacrine species,
wherein a basic uric acid structure has been partially or fully
methylated in 2, 3 or 4 positions; and b) at least one aqueous
buffered solution having a pH range of about 1.5-9.0.
2. A composition according to claim 1 wherein said theacrine, or
theacrine species are present in said aqueous composition in any
amount between about 0.01% and about 10% by weight based on the
total weight of said composition, including all percentages and
ranges of percentages therebetween.
3. A composition according to claim 1, further comprising one or
more nutritional adjuvant materials selected from the group
consisting of: flavoring agents, colorants, viscosity modifiers,
preservatives, fragrances, amino acids and their salts, vitamins,
minerals, essential fatty acids, enzymes, co-enzymes,
mono-glycerides, di-glycerides, tri-glyceride ester oils
emulsifiers, hydrolyzed proteins, whey protein, stabilizers, flow
modifiers, viscosity improvers, chelating agents, anti-oxidants,
anti-microbials, benzoates, alcohols, esters of para-hydroxybenzoic
acid, propionates, preservatives, surfactants, including anionic,
cationic or nonionic surfactants, or combinations thereof.
4. A composition according to claim 3 wherein the total amount of
said one or more nutritional adjuvant materials present is present
in any amount between about 0.01% and about 10% by weight based on
the total weight of said composition.
5. A composition according to claim 1 further comprising one or
more natural beverages, including, milk products, soy products, ice
cream, yoghurt, citrus fruit juices, non-citrus fruit juices,
vegetable juices, components of any of the foregoing, or
combinations thereof.
6. A composition according to claim 5 wherein said one or more
natural beverages is present in any amount between about 0.1% and
about 99% by weight based on the total weight of said
composition.
7. A composition according to claim 1, comprising an anti-microbial
preservative present in an effective amount to inhibit microbial
growth.
8. A composition according to claim 7 wherein said preservative
comprises a preservative selected from the group consisting of: one
or more esters of para-hydroxy benzoic acid, propionates, and one
or more sorbate salts.
9. A method for administering a bioactive form of theacrine to a
mammalian subject said method comprising the steps of: preparing a
composition according to claim 1; and orally administering said
composition.
10. The method of claim 9 wherein said method further comprises
increasing locomotor activity in the mammalian subject.
11. The method of claim 10, wherein said increasing locomotor
activity is maintained for extended time by chronic oral
administration of said composition to the mammalian subject.
12. The method of claim 9 further comprising providing enhanced
activity levels in a dose-dependent manner in the mammalian
subject.
13. The method of claim 9 further comprising reducing inflammation
in the mammalian subject.
14. The method of claim 9 further comprising reducing pain of the
mammalian subject.
15. The method of claim 9 further comprising increasing endurance
in the mammalian subject.
16. The method of claim 9 further comprising reducing depression in
the mammalian subject.
17. The method of claim 9 further comprising alleviating the
deleterious effects of hypergycemia in the mammalian subject.
18. The method of claim 9 further comprising alleviating the
deleterious effects of sleep deprivation in the mammalian
subject.
19. The method of claim 9 further comprising administering one or
more of purine alkaloids in combination with at least one
psychostimulant.
20. The method of claim 9, wherein said step of orally
administering comprises chronic or acute administration of a
composition to the mammalian subject.
Description
INDEX TO RELATED APPLICATIONS
[0001] This application is a non-provisional of, and claims benefit
to U.S. Provisional Patent Application Ser. No. 61/944,528 filed
Feb. 25, 2014 the disclosure of which is incorporated herein by
reference in its entirety.
TECHNICAL FIELD
[0002] This disclosure of the present invention relates generally
to new chemical entities (NCEs), which are a purine alkaloid
compound structurally related to caffeine and abundantly present in
Camellia kuchu, Camellia sinensis and several Coffea species. The
disclosure relates more specifically to 1,3,7,9-tetramethyluric
acid (theacrine), (O(2), 2-Methoxy-1,9-dimethyl-7H-purine-6,8-dione
(liberine) and (O(2), 1,7,9-trimethyluric acid (methylliberine)
wherein a basic uric acid structure has been partially or fully
methylated in 2, 3 or 4 positions. This disclosure relates
specifically to theacrine, and theacrine species such as liberine,
and methylliberine and compositions thereof.
[0003] The disclosure of the present invention includes synthetic
procedures of 1,3,7,9-tetramethyluric acid, O(2), 1,9-trimethyluric
acid and O(2), 1,7,9-trimethyluric acid and their subsequent
purification to yield compounds which are 99.9% pure and melting
points of 228.9.degree. C., 220.degree. C. and 215.degree. C.
respectively.
[0004] The disclosure of the present invention further relates to
compositions of matter wherein one or more of the purine alkaloid
compounds is administered to mammals in combination with other
psychostimulants including, but not limited to caffeine,
theobromine, theophylline, yohimbine, combinations thereof, and
other compounds known in the art to impart a psychostimulant
effect.
[0005] In addition this disclosure of the present invention relates
to nutritional supplements, in powder, tablet or capsule dosage
forms, aqueous formulations, containing one or more of the purine
bioactive compounds described.
[0006] In addition this disclosure of the present invention relates
to nutritional supplements, in powder, tablet or capsule dosage
forms, as solutions or suspensions, aqueous formulations, which may
be used as stimulant of the central nervous system and metabolic
stimulant. It may also be used medically to increase locomotor
activity, increase, maintain and extend locomotor activity, enhance
activity levels in a dose-dependent manner, reduce inflammation,
reduce pain, increase endurance, reduce depression, impart a
beneficial hypoglycemic effect and alleviate sleep deprivation.
BACKGROUND
[0007] Many stimulant nutritional supplements are available at
various retail outlets, in many dosage forms, including tablets,
capsules, powders, and liquids intended for human consumption. Most
of them feature caffeine as the main stimulant. Theacrine offers
the advantages of caffeine with the addition of the other benefits
included in the summary below:
SUMMARY OF THE INVENTION
[0008] Some of the benefits of the present invention include:
[0009] Theacrine increases locomotor activity. [0010] Theacrine)
increases locomotor activity and maintains it for extended time.
[0011] Theacrine enhances activity levels in a dose-dependent
manner. [0012] Theacrine reduces inflammation. [0013] Theacrine
reduces pain. [0014] Theacrine increases endurance. [0015]
Theacrine decreases depression. [0016] Theacrine alleviates sleep
deprivation. [0017] During sleep deprivation with
moderate-intensity exercise, theacrine supplementation may improve
performance of complex central executive tasks. [0018] Theacrine in
combination with other psychostimulants has a synergistic effect
that enhances the benefits described above. [0019] Theacrine may
impart a beneficial hypoglycemic effect in the management of
hyperglycemia.
[0020] The synthesis of theacrine is achieved as follows: Theacrine
is synthesized from uric acid by one step. At the presence of
potassium carbonate, uric acid is methylated by trimethyl phosphate
to give theacrine.
[0021] The one step pathway is depicted below:
##STR00001##
[0022] Stable aqueous compositions of matter useful for oral
administration of at least one biologically-active form of a purine
alkaloid compound structurally related to caffeine to a mammalian
subject, which compositions comprise: [0023] a)
1,3,7,9-tetramethyluric acid (theacrine), (O(2), 1,9-trimethyluric
acid *******PLEASE CHECK THIS****** The first character did not
save and I AM UNABLE TO LOCATE "IBERTINE" (ibertine) and (O(2),
1,7,9-trimethyluric acid (methylliberine) wherein a basic uric acid
structure has been partially or fully methylated in 2, 3 or 4
positions [0024] b) Water; [0025] c) Water (pH range of 2.0-8.5);
and [0026] d) Aqueous buffer solutions (pH range: 1.5-9.0).
[0027] In one embodiment, the present invention provides stable
aqueous compositions of matter useful for oral administration of at
least one biologically-active form of a purine alkaloid compound
structurally related to caffeine to a mammalian subject, which
compositions comprise: [0028] a) 1,3,7,9-tetramethyluric acid
(theacrine), (O(2), 2-Methoxy-1,9-dimethyl-7H-purine-6,8-dione
(liberine) and (O(2), 1,7,9-trimethyluric acid (methylliberine)
wherein a basic uric acid structure has been partially or fully
methylated in 2, 3 or 4 positions [0029] b) Aqueous buffered
solutions (pH range: 1.5-9.0).
[0030] In one embodiment, the composition provides said theacrine,
or the theacrine species (as used, theacrine species includes
liberine and methylliberine) are present in said aqueous
composition in any amount between about 0.01% and about 10% by
weight based on the total weight of said composition, including all
percentages and ranges of percentages therebetween.
[0031] In one embodiment, the composition of the present invention
is further comprising one or more nutritional adjuvant materials
selected from the group consisting of: flavoring agents, colorants,
viscosity modifiers, preservatives, fragrances, amino acids and
their salts, vitamins, minerals, essential fatty acids, enzymes,
co-enzymes, mono-glycerides, di-glycerides, tri-glyceride ester
oils emulsifiers, hydrolyzed proteins, whey protein, stabilizers,
flow modifiers, viscosity improvers, chelating agents,
anti-oxidants, anti-microbials, benzoates, alcohols, esters of
para-hydroxybenzoic acid, propionates, preservatives, surfactants
(including anionic, cationic or nonionic surfactants) or
combinations thereof.
[0032] In one embodiment, the composition of the present invention
the total amount of said one or more nutritional adjuvant materials
present is present in any amount between about 0.01% and about 10%
by weight based on the total weight of said composition.
[0033] In one embodiment, the composition of the present invention
is further comprising one or more natural beverages, including
without limitation, milk products, soy products, ice cream,
yoghurt, citrus fruit juices, non-citrus fruit juices, and
vegetable juices, or components of any of the foregoing.
[0034] In one embodiment, the composition of the present invention
has said one or more natural beverages is present in any amount
between about 0.1% and about 99% by weight based on the total
weight of said composition.
[0035] In one embodiment, the composition of the present invention
is comprising an anti-microbial preservative present in an
effective amount to inhibit microbial growth.
[0036] In one embodiment, the composition of the present invention
comprises a preservative selected from the group consisting of: one
or more esters of para-hydroxy benzoic acid, propionates, one or
more sorbate salts, or combinations thereof.
[0037] The present invention also contemplates a method for
administering a bioactive form of theacrine to a mammalian subject,
said method comprising the steps of: preparing a composition
according to the present invention; and orally administering the
composition to said mammalian subject.
[0038] The present invention also contemplates a method for
increasing locomotor activity in a mammalian subject, said method
comprising the steps of: preparing a composition according to the
present invention; and orally administering the composition to said
mammalian subject.
[0039] The present invention also contemplates a method for
increasing locomotor activity and maintaining for extended time
this activity in a mammalian subject, said method comprising the
steps of: preparing a composition according to the present
invention; and orally administering the composition to said
mammalian subject.
[0040] The present invention also contemplates a method for
enhanced activity levels in a dose-dependent manner in a mammalian
subject, said method comprising the steps of: preparing a
composition according to the present invention; and orally
administering the composition to said mammalian subject.
[0041] The present invention also contemplates a method for
reducing inflammation in a mammalian subject, said method
comprising the steps of: preparing a composition according to the
present invention; and orally administering the composition to said
mammalian subject.
[0042] The present invention also contemplates a method for
reducing pain of a mammalian subject, said method comprising the
steps of: preparing a composition according to the present
invention; and orally administering the composition to said
mammalian subject.
[0043] The present invention also contemplates a method for
increasing endurance in a mammalian subject, said method comprising
the steps of: preparing a composition according to the present
invention; and orally administering the composition to said
mammalian subject.
[0044] The present invention also contemplates a method for
reducing depression in a mammalian subject, said method comprising
the steps of: preparing a composition according to the present
invention; and orally administering the composition to said
mammalian subject.
[0045] The present invention also contemplates a method for
alleviating the deleterious effects of hypergycemia in a mammalian
subject, said method comprising the steps of: preparing a
composition according to the present invention; and orally
administering the composition to said mammalian subject.
[0046] The present invention also contemplates a method for
alleviating the deleterious effects of sleep deprivation in a
mammalian subject, said method comprising the steps of: preparing a
composition according to the present invention; and orally
administering the composition to said mammalian subject.
[0047] The present invention also contemplates a method in a
mammalian subject, said method comprising the steps of: preparing a
composition according to the present invention; and orally
administering the composition to said mammalian subject wherein the
administering is of one or more of purine alkaloids described
herein in combination with other psychostimulants in any possible
proportion in order to further enhance the benefits according to
the methods of the present invention.
[0048] As contemplated herein, the method steps of orally
administering, in one embodiment, further comprises the chronic
administration of a composition according to a mammalian
subject.
[0049] As contemplated herein, the method steps of orally
administering, in one embodiment, further comprises the acute
administration of a composition according to a mammalian
subject.
[0050] The Table 1 below is data indicating assay results for
stability of a theacrine solution prepared at 1.3 mg/ml and stored
in USP Type I Glass vials for 15 weeks at RT and 40.degree. C.
TABLE-US-00001 TABLE 1 Theacrine Stability Data Initial 1-wk 2-wk
4-wk 8-wk 15-wk Storage: Room Temperature (RT) Assay 99.6 98.7
100.1 99.2 99.9 99.3 Storage: 40 C. Assay 99.6 98.2 98.9 98.7 98.6
98.0
[0051] Table 2 below shows data indicating assay values of
theacrine solutions at 0.1%, 0.2% and 0.4% stored in USP type I
glass vials for 3 months at 40.degree. C.
TABLE-US-00002 TABLE 2 Theacrine Stability Data Storage: 40 C.
Initial 10-d 1-M 2-M 3-M 0.1% Solution 100.6 100.4 101 100.4 100.7
0.2% Solution 99.8 98.6 98.9 97.5 99.4 0.4% Solution 94.1 92.3 94.9
95.3 95.8
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
[0052] The present invention provides aqueous compositions of
matter suitable for oral administration to mammalian subjects,
including without limitation humans, which compositions comprise
theacrine species in solid or in liquid vehicles (carriers) that
have been synthesized in commercial quantities by Vital
Pharmaceuticals, Inc., d/b/a VPX/Redline of Davie, Fla.; theacrine
itself has the general structure:
##STR00002##
TABLE-US-00003 Properties Molecular formula
C.sub.9H.sub.12N.sub.4O.sub.3 Chemical name 1,3,7,9-Tetramethyluric
acid Molar mass 224.21 g/mol CAS Registry Number 2309-49-1
[0053] The material described by Structure I above, and the
corresponding text in the description, including any and all of
their derivative chemical forms, are all theacrine species and are,
as such, the subject of the present disclosure.
[0054] Aqueous compositions of matter suitable for oral
administration to mammalian subjects according to this disclosure
may be caused to have any pH in the range of between about 1.5 and
about 8.5 as desired, by adjusting such compositions using
additions of appropriate amounts of strong or weak acids or bases
including without limitation aqueous mineral acids including HCl,
H3PO4, and bases including sodium hydroxide, ethanolamines,
etc.
[0055] To prepare a composition according to one embodiment of the
present invention, one may simply add a desired amount of theacrine
to a selected volume of water, and sufficient stirring is affected
to cause dissolution of the theacrine to afford an aqueous
composition. Furthermore, according to one embodiment, the solution
may be buffered before the addition of theacrine or the solution
may be may be made more acidic or alkaline prior to the addition of
theacrine. According to another embodiment, the total concentration
of theacrine species in an aqueous solution provided hereby may be
any amount between about 0.01% and about 20% (or more) by weight
based on the total weight of the aqueous solution, including all
percentages and ranges of percentages therebetween. According to
another embodiment, the total concentration of theacrine in an
aqueous solution provided hereby may be any amount between about
0.1% and about 20% by weight based on the total weight of the
aqueous solution, including all percentages and ranges of
percentages therebetween. According to another embodiment, the
total concentration of theacrine species in an aqueous solution
provided hereby may be any amount between about 0.1% and about 25%
by weight based on the total weight of the aqueous solution,
including all percentages and ranges of percentages therebetween.
According to another embodiment, the total concentration of
Theacrine species in an aqueous solution provided hereby may be any
amount between about 0.1% and about 30% by weight based on the
total weight of the aqueous solution, including all percentages and
ranges of percentages therebetween. In an alternate embodiment,
theacrine (or any one or more theacrine species) may be added to a
natural beverage in any amount provided that an aqueous solution or
suspension results.
[0056] In addition, a composition according to the present
invention also includes nutritional adjuvant materials including
flavoring agents, colorants, viscosity modifiers, preservatives,
chelating agents, antioxidants, surface modifiers and other
nutritional adjuvant materials. Other nutritional adjuvant
materials include any substance which is generally recognized as
promoting the health or function of a mammalian organism, including
humans, or benefiting a composition useful thereof in terms of its
efficacy, appearance, stability, consistency, aroma, or viscosity.
Such substances include, but are not limited to, other amino acids
and their salts, vitamins, minerals, essential fatty acids,
enzymes, mono-glycerides, di-glycerides, tri-glyceride ester oils
(including, for example vegetable oils and animal fats)
emulsifiers, hydrolyzed proteins, whey protein, stabilizers, flow
modifiers, viscosity improvers, chelating agents, enzymes,
surfactants, whether anionic, cationic or nonionic, and
combinations thereof. The total amount of the one or more
nutritional adjuvant materials above present in a composition
according to this disclosure is present in any amount between about
0.01% and about 50% by weight based on the total weight of said
composition, including all percentages and ranges of percentages
therebetween.
[0057] In addition to ingredients containing adjuvant materials, a
composition according to one embodiment of the present invention
also comprises one or more natural beverages. A natural beverage,
as used herein, is a beverage suitable for human or animal
consumption which contains the pulp, juice or any other constituent
of a naturally-occurring fruit, vegetable, or animal product
whether from the wild, cultured, cultivated on a farm or otherwise
domesticated by Man. Natural beverages include without limitation
materials including, but not limited to as milk products, soy
products, ice cream, yoghurt, citrus fruit juices, non-citrus fruit
juices, and vegetable juices, or components of any of the
foregoing, wherein said natural beverages are present in any
effective amount to impart flavor to the compositions, which are
any amount between about 0.1% and about 99% by weight based on the
total weight of said composition, including all percentages and
ranges of percentages there between.
[0058] In addition to ingredients containing adjuvant materials, a
composition according to one embodiment of the present invention
comprises one or more synthetic beverages. A synthetic beverage is
any beverage that is not a natural beverage.
[0059] In general, a composition according to one embodiment of the
present invention is provided by combining and mixing the
ingredients selected, including theacrine and any desired quantity
of any one or more other ingredients specified herein. One
advantage of compositions according to this disclosure is that they
may be packaged at pH levels as low as about pH 2, in the cold or
at about room temperature (alternative embodiment) or only slightly
elevated temperature (alternative embodiment), as opposed to many
prior art compositions which typically require hot packaging
methods that utilize specialized and expensive equipment and
packaging materials.
[0060] Thus, it is evident that a composition according to one
embodiment of the present invention is made quite palatable by a
mammalian subject, including human subjects desiring to administer
theacrine orally in an aqueous mixture. Typical serving sizes may
be any serving size in the range of about 1 milligram to about 50
grams, in an aqueous solution that is from about 20 ml to about
2500 ml in volume. The composition of theacrine in an aqueous
composition according to this disclosure is limited only by the
solubility limit of the theacrine and which may exceed 50 grams per
liter and concentrations at or near the solubility limit are herein
provided by contacting excess amounts of the theacrine in contact
with water or an aqueous solution to provide a solution saturated
with theacrine. Such saturated solutions may then be diluted
slightly, to afford a concentrate from which other theacrine
containing compositions may be conveniently provided.
Descriptions of Compositions
[0061] The following compositions are illustrative and not meant to
limit the scope of the present invention.
[0062] 1. An oral liquid composition (Ready-to-Drink) comprising
Theacrine, said composition with a pH of about 2 to 8.5 being
substantially stable at room temperature for normal warehouse
storage conditions, stable at 104.degree. F. (40 C. degrees) for
shipping in hot weather trucks and/or overseas containers, and
stable at 39.degree. F. (4 C. degrees) in coolers so that it can be
stored under refrigeration conditions. The composition comprising a
suitable aqueous solvent or vehicle, a non-aqueous vehicle, a
preservative, a physical stabilizing ingredient, one or more
surfactants, and one or more buffer salts that can render the
composition pH stable. The composition, in one embodiment contains
psychostimulants, nucleotides, oligonucleotides, the
monophosphates, diphosphates, triphosphates and cyclic derivatives
of these nucleotides, and amino acids, vitamins and vitamin-like
isoprenoids, peptides and one or more additional components
selected from the group consisting of: lipids, starches,
carbohydrates, polyols, minerals, electrolytes, amino trace
elements, colorings, flavors, artificial sweeteners, and
anti-oxidants.
[0063] 2. An oral liquid composition for buccal sublingual
administration comprising Theacrine, said composition with a pH of
about 2 to 8.5 being substantially stable at room temperature for
normal warehouse storage conditions, stable at 104.degree. F. (40
C. degrees) for shipping in hot weather trucks and/or overseas
containers, and stable at 39.degree. F. (4 C. degrees) in coolers
so that it can be stored under refrigeration conditions. The
composition comprising a suitable aqueous solvent or vehicle, a
non-aqueous vehicle, a preservative, a physical stabilizing
ingredient, one or more surfactants, and one or more buffer salts
that can render the composition pH stable. The composition, in one
embodiment, contains psychostimulants, nucleotides,
oligonucleotides, the monophosphates, diphosphates, triphosphates
and cyclic derivatives of these nucleotides, and amino acids,
vitamins and vitamin-like isoprenoids, peptides and one or more
additional components selected from the group consisting of:
lipids, starches, carbohydrates, polyols, minerals, electrolytes,
amino trace elements, colorings, flavors, artificial sweeteners,
and anti-oxidants.
[0064] 3. An oral solid composition in the form of a capsule
(LiCap.RTM.) with a liquid composition as fill material, said
liquid fill material being substantially stable at room temperature
for normal warehouse storage conditions, stable at 104.degree. F.
(40 C. degrees) for shipping in hot weather trucks and/or overseas
containers, and stable at 39.degree. F. (4 C. degrees) in coolers
so that it can be stored under refrigeration conditions. The
composition comprising a suitable lipophilic solvent or vehicle, a
physical stabilizing ingredient, one or more surfactants, and one
or more buffer salts that can render the composition pH stable. The
composition in one embodiment, contains psychostimulants,
nucleotides, oligonucleotides, the monophosphates, diphosphates,
triphosphates and cyclic derivatives of these nucleotides, and
amino acids, vitamins and vitamin-like isoprenoids, peptides and
one or more additional components selected from the group
consisting of: lipids, medium and short chain triglycerides,
starches, polyols, carbohydrates, minerals, electrolytes, amino
trace elements, colorings, and anti-oxidants.
[0065] 4. An oral liquid composition containing from 1 gram to 100
grams of protein and from 1 g ram to 100 g of carbohydrates per
serving comprising Theacrine, said liquid being substantially
stable at room temperature for normal warehouse storage conditions,
stable at 104.degree. F. (40 C. degrees) for shipping in hot
weather trucks and/or overseas containers, and stable at 39.degree.
F. (4 C. degrees) in coolers so that it can be stored under
refrigeration conditions. The composition comprising an acid stable
protein isolates, or a combination or blend of protein isolates,
concentrates and hydrolyzates and caseins in micellar forms, a
suitable aqueous solvent or vehicle, a non-aqueous vehicle, a
preservative, a physical stabilizing ingredient, one or more
surfactants, and one or more buffer salts that can render the
composition pH stable. The composition, in one embodiment, contains
psychostimulants, nucleotides, oligonucleotides, the
monophosphates, diphosphates, triphosphates and cyclic derivatives
of these nucleotides, and amino acids, vitamins and vitamin-like
isoprenoids, peptides and one or more additional components
selected from the group consisting of: lipids, starches,
carbohydrates, polyols, minerals, electrolytes, amino trace
elements, colorings, flavors, artificial sweeteners, and
anti-oxidants.
[0066] 5. An aqueous injectable composition for human consumption
said composition being isotonic and sterile in nature comprising
Theacrine, said injectable preparation with a pH of about 2, being
substantially stable at room temperature for normal warehouse
storage conditions, stable at 104.degree. F. (40 C. degrees) for
shipping in hot weather trucks and/or overseas containers, and
stable at 39.degree. F. (4 C. degrees) in coolers so that it can be
stored under refrigeration conditions. The composition comprising a
suitable aqueous solvent, a preservative, a physical stabilizing
ingredient and one or more buffer salts that can render the
composition pH stable. The composition, in one embodiment, contains
psychostimulants, nucleotides, oligonucleotides, the
monophosphates, diphosphates, triphosphates and cyclic derivatives
of these nucleotides, and amino acids, peptides, proteins and
carbohydrates.
[0067] 6. An emulsion injectable composition for human consumption
said composition being isotonic and sterile in nature comprising
Theacrine, said injectable preparation with a pH of about 2, being
substantially stable at room temperature for normal warehouse
storage conditions, stable at 104.degree. F. (40 C. degrees) for
shipping in hot weather trucks and/or overseas containers, and
stable at 39.degree. F. (4 C. degrees in coolers so that it can be
stored under refrigeration conditions. The composition comprising a
suitable aqueous solvent, pharmaceutically acceptable oil (sesame,
olive, castor, peanut, cotton seed, etc.), a natural emulsifier
such as lecithin or any other synthetic emulsifier, be it of the
polysorbate or ethoxylated glyceride type, a preservative, a
physical stabilizing ingredient and one or more buffer salts that
can render the composition pH stable. The composition, in one
embodiment, contains psychostimulants, nucleotides,
oligonucleotides, the monophosphates, diphosphates, triphosphates
and cyclic derivatives of these nucleotides, and amino acids,
peptides, proteins and carbohydrates.
EXAMPLES
Ready to Drink Formulation
Example I
TABLE-US-00004 [0068] INGREDIENTS (Ready-to-Drink Formulation) %
w/w Purified water 97.1 Theacrine 1.00 Caffeine 2.00 Gamma
Butyrobetaine 0.0156 Glycerin 1.067 Anserine 0.052 Caffeine 0.06
Magnesium Tanshinoate 0.0000009 L-Leucine 0.104 L-Isoleucine 0.052
L-Valine 0.0208 1,3-di-n-propyl-7-propargylxanthine 1E-10
Geranamine 0.0004 Citric acid to pH 3.33 0.179 Sodium benzoate
0.052 Potassium sorbate 0.01 Bis picolinate vanadium 0.0000002 Salt
0.005 Potassium phosphate dibasic 0.0206 Sodium Erythorbate
0.000001 Nisaplin 0.000001 Sucralose 0.073 Malic acid 0.083 Flavor
Melon 0.105
Example II
TABLE-US-00005 [0069] INGREDIENTS % w/w Theacrine 2.10 Caffeine
4.20 Peptides 3.00 AMP 12.50 UTP 0.10 Ubiquinone 3.20
Ethoxydiglycol 20.0 Alcohol USP 50.0 Benzyl alcohol 1.00 Buffer
Salt(s) QS to adjust pH Purified Water QS to 100
Example III
TABLE-US-00006 [0070] INGREDIENTS % w/w Theacrine 2.10 Caffeine
4.20 Peptides 3.00 AMP 12.50 UTP 0.10 Ubiquinone 3.20 Propylene
Glycol 20.0 Alcohol USP 40.0 Polysorbate 80 5.0 Benzyl alcohol 1.00
Buffer Salt(s) QS to adjust pH Purified Water QS to 100
Fill Material Composition for Capsule
Example I
TABLE-US-00007 [0071] INGREDIENTS % w/w Theacrine 2.10 Medium chain
triglyceride 15.0 Peptides 3.00 AMP 12.50 UTP 0.10 Ubiquinone 3.30
Oleic Acid 52.0 Purified Water 1.0-10.0
Example II
TABLE-US-00008 [0072] INGREDIENTS % w/w Theacrine 2.10 Peptides
3.00 AMP 12.50 UTP 0.10 Ubiquinone 3.30 Polysorbate 80 25.0 PEG-40
Hydrogenated Castor Oil 38.00 PEG esters and monoglycerides 15.0
Purified Water QS to 100
Example III
TABLE-US-00009 [0073] INGREDIENTS % w/w Theacrine 2.10 Peptides
3.00 AMP 12.50 UTP 0.10 Ubiquinone 3.30 PEG-400 45.0 PEG esters and
monoglycerides 9.00 Polysorbate 80 20.0 Buffer Salt(s) QS to adjust
pH Purified Water QS to 100
Medium Range pH RTD Protein Blend Formulations
TABLE-US-00010 [0074] Ingredient % w/w Per 16 oz Serving Theacrine
1.00 2.10 Whey Protein Isolate 6.000 30.00 Whey Protein Concentrate
0.640 3.20 Whey Hydrolysate 0.320 1.60 Micellar casein 0.320 1.60
Casein Protein Hydrolysate 0.000 0.00 Potassium Chloride 0.076 0.38
Ascorbic Acid 0.012 0.06 Vitamin E TPGS 0.052 0.26 Riboflavin 100
0.000 0.00000010 Niacin 0.000 0.0020 Pyrodoxine HCl 0.000 0.000007
Calcium Panthothenate 0.000 0.0011 Magnesium Maleate 0.020 0.1000
d-ribose 0.040 0.2000 Centromix E 0.600 3.00 Saflower Oil 1.200
6.00 Sunflower Oil 1.200 6.00 Medium Chain Triglycerides 0.800 4.00
L-Glutamine 0.025 0.13 Glucose Polymers (Rice trin) 0.800 4.00 Waxy
Maize Starch 1.000 5.00 High Amylose Starch (Amylose ADP11P) 0.100
0.50 Magnesium Citrate 0.124 0.62 Microcrystalline Cellulose 0.100
0.50 Malic Acid 0.140 0.70 Citric acid to pH 6.5 0.566 2.83 Sodium
Citrate to pH 6.5 0.140 0.70 Sucralose 0.011 0.06 Glycerin 3.000
15.00 Na 2 EDTA 0.050 0.25 Sodium Benzoate 0.090 0.45 Potassium
Sorbate 0.190 0.95 Water QS QS
Low pH RTD Protein Formulations
TABLE-US-00011 [0075] Per 16 oz serving % w/w Theacrine 2.10 0.25
Whey Protein Isolate Acid Stable 44.44 9.26 Sucralose 0.12 0.025
Sodium EDTA 0.24 0.050 Potassium Sorbate 0.96 0.200 Sodium Benzoate
0.48 0.100 Citric Acid to pH 3.0 QS QS Malic Acid to pH 3.0 QS QS
Water 433.8 90.37 480 100
Low pH RTD Protein Formulations
TABLE-US-00012 [0076] Per 16 oz serving % w/w Theacrine 2.10 0.25
Whey Protein Isolate Acid Stable 44.44 9.26 Sucralose 0.12 0.025
Waxy Maize Starch 4.80 1.00 Glucose Polymers (Rice trin) 0.96 0.20
Na EDTA 0.24 0.050 Potassium Sorbate 0.96 0.200 Sodium Benzoate
0.48 0.100 Citric Acid to pH 3.0 QS QS Malic Acid to pH 3.0 QS QS
Water QS QS TOTAL 480 100
Aqueous Injectable Formulations
Example I
TABLE-US-00013 [0077] Ingredient % w/v Theacrine 6.25 Caffeine 12.5
AMP 12.5 UTP 0.10 Amino Acids 3.0-7.0 Polysorbate 80 0.40 Sodium
CMC 0.50 Sodium Chloride 0.90 Benzyl alcohol 0.90 Buffer Salt(s) QS
to adjust to pH 3--6.5 Sodium Hydroxide QS to adjust to pH 3-6.5
Water for Injection QS to 100
Example II
TABLE-US-00014 [0078] Ingredient % w/v Theacrine 6.25 Caffeine
12.50 UTP 0.10 Amino Acids 3.0-7.0 Polysorbate 80 0.40 Sorbitol
40.00 Sodium Chloride 0.90 Benzyl alcohol 0.90 Buffer Sat(s) QS to
adjust to pH 3--6.5 Sodium Hydroxide QS to adjust to pH 3-6.5 Water
for Injection QS to 100
Example III
TABLE-US-00015 [0079] Ingredient % w/v Theacrine 6.25 Caffien 12.5
Polysorbate 80 0.40 AMP 12.50 UTP 0.10 Amino Acids 3.0-7.0 Sodium
Citrate 0.50 Sodium Chloride 0.90 Benzyl alcohol 0.90 Buffer
Salt(s) QS to adjust to pH 3--6.5 Sodium Hydroxide QS to adjust to
pH 3-6.5 Water for Injection QS to 100
Emulsion Injectable Formulations
Example I
TABLE-US-00016 [0080] Ingredient % w/v Theacrine 6.25 Caffeine 12.5
AMP 12.5 UTP 0.10 Amino Acids 3.0-7.0 Sesame Oil 2.0-12.0
Polysorbate 80 0.40 Sodium Chloride 0.90 Benzyl alcohol 0.90 Buffer
Salt(s) QS to adjust to pH 3--6.5 Sodium Hydroxide QS to adjust to
pH 3-6.5 Water for Injection QS to 100
Example II
TABLE-US-00017 [0081] Ingredient % w/v Theacrine 6.25 Caffeine 12.5
AMP 12.50 UTP 0.10 Amino Acids 3.0-7.0 Olive Oil 1.0-15.0 Lecithin
0.50-5.0 Sorbitol 30.00 Sodium Chloride 0.90 Benzyl alcohol 0.90
Buffer Sat(s) QS to adjust to pH 3-6.5 Sodium Hydroxide QS to
adjust to pH 3-6.5 Water for Injection QS to 100
Example III
TABLE-US-00018 [0082] Ingredient % w/v Theacrine 6.25 Caffeine 12.5
Peanut Oil 1.0-15.0 Polysorbate 80 0.2-10.0 AMP 12.50 UTP 0.10
Amino Acids 3.0-7.0 Sodium Citrate 0.50 Sodium Chloride 0.90 Benzyl
alcohol 0.90 Buffer Salt(s) QS to adjust to pH 3--6.5 Sodium
Hydroxide QS to adjust to pH 3-6.5 Water for Injection QS to
100
[0083] A composition as provided herein may be administered
chronically. As used herein, "chronically" has its normal meaning,
which generally means repeated ingestion over a period of several
days, several weeks or even several months. "Chronic" is generally
not acute.
[0084] Consideration must be given to the fact that although this
disclosure has been described and disclosed in relation to certain
preferred embodiments, obvious equivalent modifications and
alterations thereof will become apparent to one of ordinary skill
in this art upon reading and understanding this specification and
the claims appended hereto. This includes subject matter defined by
any combination of any one of the various claims appended hereto
with any one or more of the remaining claims, including the
incorporation of the features and/or limitations of any dependent
claim, singly or in combination with features and/or limitations of
any one or more of the other dependent claims, with features and/or
limitations of any one or more of the independent claims, with the
remaining dependent claims in their original text being read and
applied to any independent claims so modified. This also includes
combination of the features and/or limitations of one or more of
the independent claims with features and/or limitations of another
independent claim to arrive at a modified independent claim, with
the remaining dependent claims in their original text being read
and applied to any independent claim so modified. Accordingly, the
present disclosure is intended to cover all such modifications and
alterations and is not intended to be necessarily limited by any
one or more particular strict interpretations of the claims that
now follow.
* * * * *